title: Comparative in vitro activities of rifamycin analogues against Mycobacterium leprae.
abstract: Comparative activities of various rifamycin analogues against leprosy were studied by evaluating their effects on in vitro growth of Mycobacterium leprae in DH medium as described earlier. Among the seven analogues studied, KRM-1648 was found to be the most potent in inhibiting the growth of rifampicin-sensitive strains of M. leprae, MIC being 0.05 microgram/ml. This was followed by KRM-2312 and T9 (MIC of each being 0.1 microgram/ml) and rifabutin (MIC, 0.2 microgram/ml). Rifampicin, along with KRM-1657 and KRM-1668, were least effective, with MIC for each being 0.4 microgram/ml. The effects of each at their respective MICs were bactericidal. The results were similar for rifampicin-resistant strains of M. leprae, but the MICs were higher than those obtained with rifampicin-sensitive strains of M. leprae. Thus, even though rifampicin has been the first-line drug in the treatment of leprosy, the results in present studies suggest that other rifamycin analogues are available that are more potent than rifampicin against both rifampicin-sensitive as well as rifampicin-restraint strains of M. leprae.
authors.affiliation: Department of Biological Sciences, Florida Institute of Technology Melbourne 32901, USA.
authors.forename: A M
authors.initials: AM
authors.lastname: Dhople
mesh_terms: D004352:Drug Resistance, Microbial; D007917:Leprostatic Agents / Q000494:pharmacology*; D009166:Mycobacterium leprae / Q000187:drug effects*; D012293:Rifampin / Q000031:analogs & derivatives* / Q000494:pharmacology*
chemical_list: D007917:Leprostatic Agents; D012293:Rifampin